- Microwave use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds method
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The invention discloses a microwave the use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds, in the aqueous phase under microwave conditions adding benzoic amidine compound under alkaline condition [...] into benzimidazole reaction, invention an environment-friendly, the operation is simple, cheap and safe, efficient process for preparing benzimidazole method. Compared with the prior art, this method not only can be applied to a large number of functional groups, the productive rate is high, few by-products, and the operation is simple, safe, low cost, environmental protection; .
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Paragraph 0067
(2019/03/28)
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- Anaerobic 5-Hydroxybenzimidazole Formation from Aminoimidazole Ribotide: An Unanticipated Intersection of Thiamin and Vitamin B12 Biosynthesis
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Comparative genomics of the bacterial thiamin pyrimidine synthase (thiC) revealed a paralogue of thiC (bzaF) clustered with anaerobic vitamin B12 biosynthetic genes. Here we demonstrate that BzaF is a radical S-adenosylmethionine enzyme that catalyzes the remarkable conversion of aminoimidazole ribotide (AIR) to 5-hydroxybenzimidazole (5-HBI). We identify the origin of key product atoms and propose a reaction mechanism. These studies represent the first step in solving a long-standing problem in anaerobic vitamin B12 assembly and reveal an unanticipated intersection of thiamin and vitamin B12 biosynthesis.
- Mehta, Angad P.,Abdelwahed, Sameh H.,Fenwick, Michael K.,Hazra, Amrita B.,Taga, Michiko E.,Zhang, Yang,Ealick, Steven E.,Begley, Tadhg P.
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supporting information
p. 10444 - 10447
(2015/09/28)
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- A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
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A series of novel benzimidazoles are discussed as NR2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists. High throughput screening (HTS) efforts identified a number of potent and selective NR2B antagonists such as 1. Exploration of the substituents around the core of this template identified a number of compounds with high potency for NR2B (pIC50 >7) and good selectivity against the NR2A subunit (pIC50 2+ and radioligand binding studies. These agents offer potential for the development of therapeutics for a range of nervous system disorders including chronic pain, neurodegeneration, migraine and major depression.
- Davies, David J.,Crowe, Matthew,Lucas, Nolwenn,Quinn, Joanna,Miller, David D.,Pritchard, Sara,Grose, David,Bettini, Ezio,Calcinaghi, Novella,Virginio, Caterina,Abberley, Lee,Goldsmith, Paul,Michel, Anton D.,Chessell, Iain P.,Kew, James N.C.,Miller, Neil D.,Gunthorpe, Martin J.
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p. 2620 - 2623
(2012/05/05)
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- Mild and general one-pot reduction and cyclization of aromatic and heteroaromatic 2-nitroamines to bicyclic 2 H -imidazoles
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A one-pot procedure for the conversion of aromatic and heteroaromatic 2-nitroamines into bicyclic 2H-benzimidazoles is described. The procedure employs formic acid, iron powder, and an additive such as NH4Cl to reduce the nitro group and effect the imidazole cyclization with high-yielding conversions generally within one to two hours. The compatibility with a wide range of functionality demonstrates the general utility of this procedure.
- Hanan, Emily J.,Chan, Bryan K.,Estrada, Anthony A.,Shore, Daniel G.,Lyssikatos, Joseph P.
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experimental part
p. 2759 - 2764
(2010/12/25)
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- Highly efficient and scalable process for demethylation of 6-(2,4-dimethoxybenzoyl)chromen-2-one and other aryl methyl ethers
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Demethylation of 6-(2,4-dimethoxybenzoyl)chromen-2-one and some other aryl methyl ethers was achieved with pyridinium bromide as demethylating agent and sulfolane as solvent. Compared with other demethylation methods, this combination offers advantages of clean conversion, excellent yields, easy operation and workup, and manageable reaction temperatures. This process could be particularly useful for large-scale production because it avoids use of corrosive or moisture-sensitive reagents. Copyright
- Srivastava, Amit,Yang, Jason,Zhao, Baoshu,Jiang, Yong,Blackmon, Wade,Kraemer, Bernd
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experimental part
p. 1765 - 1771
(2010/07/07)
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- A facile one-pot synthesis of benzimidazoles from 2-nitroanilines by reductive cyclization
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A facile one-pot process to prepare benzimidazole derivatives is described. Reductive cyclization of a serial of 2-nitroanilines with orthoesters in the presence of Pd/C in methanol at room temperature, which is promoted by a catalytic amount of acetic acid, affords the corresponding benzimidazole derivatives in high yields.
- Liu, Zheng,Li, Haihong,Zhao, Qingjie,Shen, Jingshan
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scheme or table
p. 1907 - 1911
(2009/04/06)
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- ANTI-VIRAL COMPOUNDS
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Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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Page/Page column 125
(2010/11/27)
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- Rapid one-pot preparation of 2-substituted benzimidazoles from 2-nitroanilines using microwave conditions
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A high yielding one-pot procedure for the generation of 2-substituted benzimidazoles directly from 2-nitroanilines by in situ reduction and cyclization using a microwave procedure is described.
- VanVliet, David S.,Gillespie, Paul,Scicinski, Jan J.
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p. 6741 - 6743
(2007/10/03)
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- PHENYL AND HETEROCYCLIC TETRAHYDROPYRIDYL ALKOXY-BENZHETEROCYCLIC COMPOUNDS AS ANTIPSYCHOTIC AGENTS
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Novel phenyl and heterocyclic tetrahydropyridyl and piperazinyl alkoxy benzheterocyclic compounds are described which have valuable neuroleptic properties by virtue of their dopamine autoreceptor agonist activity. Methods of preparation, pharmaceutical co
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